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ADSB-FUB-187
ADSB-FUB-187 is an indazole-based synthetic cannabinoid. It is a potent agonist of the CB1 receptor with a binding affinity of ''K''i = 0.09 nM and an EC50 of 1.09 nM. It was originally developed by Pfizer in 2009, being example 187 from patent WO 2009/106982. While it is the most tightly binding compound from this patent in terms of ''K''i, it is not the most potent compound at producing a CB1 mediated pharmacological effect, with at least 17 other compounds from the patent having lower EC50 values. Legality Sweden's public health agency suggested classifying ADSB-FUB-187 as hazardous substance on November 10, 2014, following its use as an ingredient in grey-market synthetic cannabis products. See also * AB-FUBINACA * ADB-FUBINACA ADB-FUBINACA is a designer drug identified in synthetic cannabis blends in Japan in 2013. In 2018, it was the third-most common synthetic cannabinoid identified in drugs seized by the Drug Enforcement Administration. The ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ADB-FUBINACA
ADB-FUBINACA is a designer drug identified in synthetic cannabis blends in Japan in 2013. In 2018, it was the third-most common synthetic cannabinoid identified in drugs seized by the Drug Enforcement Administration. The (''S'')-enantiomer of ADB-FUBINACA is described in a 2009 Pfizer patent and has been reported to be a potent agonist of the CB1 receptor and the CB2 receptor with EC50 values of 1.2 nM and 3.5 nM, respectively. ADB-FUBINACA features a carboxamide group at the 3-indazole position, like SDB-001 and STS-135. ADB-FUBINACA appears to be the product of rational drug design, since it differs from AB-FUBINACA only by the replacement of the isopropyl group with a ''tert''-butyl group. An analogue of ADB-FUBINACA, ADSB-FUB-187, containing a more functionalized carboxamide substituent was recently reported. Side effects One death through coronary arterial thrombosis has been linked to ADB-FUBINACA intoxication. At least an additional 8 deaths in Hung ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indazole
Indazole, also called isoindazole, is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and pyrazole. Indazole is an amphoteric molecule which can be protonated to an indazolium cation or deprotonated to an indazolate anion. The corresponding ''pKa'' values are 1.04 for the equilibrium between indazolium cation and indazole and 13.86 for the equilibrium between indazole and indazolate anion. Indazole derivatives display a broad variety of biological activities. Indazoles are rare in nature. The alkaloids nigellicine, nigeglanine, and nigellidine are indazoles. Nigellicine was isolated from the widely distributed plant ''Nigella sativa'' L. (black cumin). Nigeglanine was isolated from extracts of ''Nigella glandulifera''. The Davis–Beirut reaction can generate 2''H''-indazoles. Indazole, C7H6N2, was obtained by E. Fischer (''Ann.'' 1883, 221, p. 280) by heating ortho-hydrazine cinnamic acid, : Some derivatives ; indazole-3- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synthetic Cannabinoid
Synthetic cannabinoids are a class of designer drug molecules that bind to the same receptors to which cannabinoids ( THC, CBD and many others) in cannabis plants attach. These novel psychoactive substances should not be confused with synthetic phytocannabinoids (THC or CBD obtained by chemical synthesis) or synthetic endocannabinoids from which they are in many aspects distinct. Typically, synthetic cannabinoids are sprayed onto plant matter and are usually smoked, although they have also been ingested as a concentrated liquid form in the US and UK since 2016. They have been marketed as herbal incense, or "herbal smoking blends", and sold under common names like K2, spice, and synthetic marijuana. They are often labeled "not for human consumption" for liability defense. A large and complex variety of synthetic cannabinoids are designed in an attempt to avoid legal restrictions on cannabis, making synthetic cannabinoids designer drugs. Most synthetic cannabinoids are ag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists Receptors can be activated by either agonists (such as[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CB1 Receptor
Cannabinoid receptor type 1 (CB1), also known as cannabinoid receptor 1, is a G protein-coupled cannabinoid receptor that in humans is encoded by the ''CNR1'' gene. The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. It is activated by: endocannabinoids, a group of retrograde neurotransmitters that include anandamide and 2-arachidonoylglycerol (2-AG); plant phytocannabinoids, such as the compound THC which is an active ingredient of the psychoactive drug cannabis; and, synthetic analogs of THC. CB1 is antagonized by the phytocannabinoid tetrahydrocannabivarin (THCV). The primary endogenous agonist of the human CB1 receptor is anandamide. Structure The CB1 receptor shares the structure characteristic of all G-protein-coupled receptors, possessing seven transmembrane domains connected by three extracellular and three intracellular loops, an extracellular N-terminal tail, and an intracellular C-terminal tail. The recep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Affinity
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition of lig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EC50
] Half maximal effective concentration (EC50) is a measure of the concentration of a drug, antibody or toxicant which induces a Stimulus%E2%80%93response_model, response halfway between the baseline and maximum after a specified exposure time. More simply, EC50 can be defined as the ''concentration required to obtain a 50% ..effect'' and may be also written as sub>50. It is commonly used as a measure of a drug's potency, although the use of EC50 is preferred over that of 'potency', which has been criticised for its vagueness. EC50 is a measure of concentration, expressed in molar units (M), where 1 M is equivalent to 1 mol/ L. The EC50 of a ''graded'' dose response curve therefore represents the concentration of a compound where 50% of its maximal effect is observed. The EC50 of a ''quantal'' dose response curve represents the concentration of a compound where 50% of the population exhibit a response, after a specified exposure duration. For clarification, a gra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pfizer
Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfizer (1824–1906) and his cousin Charles F. Erhart (1821–1891). Pfizer develops and produces medicines and vaccines for immunology, oncology, cardiology, endocrinology, and neurology. The company has several blockbuster drugs or products that each generate more than billion in annual revenues. In 2020, 52% of the company's revenues came from the United States, 6% came from each of China and Japan, and 36% came from other countries. Pfizer was a component of the Dow Jones Industrial Average stock market index from 2004 to August 2020. The company ranks 64th on the Fortune 500 and 49th on the Forbes Global 2000. History 1849–1950: Early history Pfizer was founded in 1849 by Charles Pfizer and Charles F. Erhart, two cousins w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synthetic Cannabis
Synthetic cannabinoids are a class of designer drug molecules that bind to the same receptors to which cannabinoids ( THC, CBD and many others) in cannabis plants attach. These novel psychoactive substances should not be confused with synthetic phytocannabinoids (THC or CBD obtained by chemical synthesis) or synthetic endocannabinoids from which they are in many aspects distinct. Typically, synthetic cannabinoids are sprayed onto plant matter and are usually smoked, although they have also been ingested as a concentrated liquid form in the US and UK since 2016. They have been marketed as herbal incense, or "herbal smoking blends", and sold under common names like K2, spice, and synthetic marijuana. They are often labeled "not for human consumption" for liability defense. A large and complex variety of synthetic cannabinoids are designed in an attempt to avoid legal restrictions on cannabis, making synthetic cannabinoids designer drugs. Most synthetic cannabinoids are agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AB-FUBINACA
AB-FUBINACA is a drug that acts as a potent agonist for the cannabinoid receptors, with ''K''i values of 0.9 nM at CB1 and 23.2 nM at CB2 and EC50 values of 1.8 nM at CB1 and 3.2 nM at CB2. It was originally developed by Pfizer in 2009 as an analgesic medication but was never pursued for human use. In 2012, it was discovered as an ingredient in synthetic cannabinoid blends in Japan, along with a related compound AB-PINACA, which had not previously been reported. Its use has been linked to hospitalizations and deaths. Legality It was designated as a Schedule I controlled substance in the United States in January 2014. It is an Anlage II controlled substance in Germany as of November 2014. Since October 2015 AB-FUBINACA is a controlled substance in China . In December 2019, the UNODC announced scheduling recommendations placing AB-FUBINACA as a controlled research chemical into Schedule II. 101789 Mass overdoses due to adulterated K2 On August 15t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoids
Cannabinoids () are several structural classes of compounds found in the cannabis plant primarily and most animal organisms (although insects lack such receptors) or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary intoxicating compound in cannabis. Cannabidiol (CBD) is a major constituent of temperate Cannabis plants and a minor constituent in tropical varieties. At least 113 distinct phytocannabinoids have been isolated from cannabis, although only four (i.e., THCA, CBDA, CBCA and their common precursor CBGA) have been demonstrated to have a biogenetic origin. It was reported in 2020 that phytocannabinoids can be found in other plants such as rhododendron, licorice and liverwort, and earlier in Echinacea. Phytocannabinoids are multi-ring phenolic compounds structurally related to THC, but endocannabinoids are fatty acid derivatives. Nonclassical synthetic cannabinoids (cannabimimetics) includ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
